Diosgenin is a major bioactive constituent of various edible pulses and roots, well characterized in the seeds of fenugreek as well as in the root tubers of wild yams. The findings from pre-clinical and mechanistic studies strongly implicate the use of diosgenin as a novel multi-target based chemo preventive or therapeutic agent against several chronic diseases. Diosgenin has been shown to increase cholesterol secretion fiveto seven-fold in the bile of rats without altering the output of bile salts and phospholipids (Kosters et al., 2005; Nervi et al., 1988; Nibbering et al., 2001). Recently, it was shown that the biliary cholesterol secretion stimulated by diosgenin and leading to fecal cholesterol excretion is independent of intestinal cholesterol absorption. The anti-cancer effects of diosgenin in vitro through different mechanisms was investigated and was shown that it could use in the treatment Colon cancer, breast cancer, prostate cancer and some others. Also was investigates the effect of diosgenin on hepatitis C virus (HCV) replication and was shown that compound can inhibits HCV replication at low µM concentrations. Diosgenin was able to protect the kidney from morphological changes associated with ovariectomy. The mechanism is responsible for this protection was the conversion of diosgenin to progesterone. The extensive pre-clinical and clinical research should be carried out prior to advocating the safe and efficacious use of diosgenin and diosgenin-rich plant extracts against the prevention and control of diseases.

Modecainide is a benzanilide derivative patented by American pharmaceutical company Bristol-Myers Co. as type Ic antiarrhythmic agent. Modecainide is a major metabolite of Encainide, a class Ic antiarrhythmic, with comparable antiarrhythmic activity. Modecainide is never marketed because of its frequent proarrhythmic side effects.

Cadazolid is a new antibiotic in development for the treatment of Clostridium difficile-associated diarrhea. Cadazolid is active against all (including linezolid- and moxifloxacin-resistant) Clostridium difficile strains. In phase I and II clinical trials, cadazolid was shown to be safe, well tolerated, and efficacious positioning itself as a potential future viable therapeutic option for CDI. Using a series of macromolecular labeling, in vitro transcription/translation, and topoisomerase studies, it was determined that protein synthesis inhibition via the oxazolidinone moiety is the primary mechanism of action of cadazolid. Cadazolid is in phase III clinical trials by Actelion Pharmaceuticals for the treatment of Clostridium difficile infection. The US FDA has designated cadazolid as both a Qualified Infectious Disease Product (QIDP) and a Fast Track development program for this indication.

Cloguanamil is an antiprotozoal agent, useful against malaria parasites. The drug was synthesized by Wellcome Research Laboratories in the 1970s.

Halofenate (MK-185) was invented as a hypolipidemic and hypouricemic agent. It was shown that halofenate lower serum triglycerides and uric acid in patients with a variety of hyperlipidemias. Treatment of dyslipidemic type 2 diabetic patients also showed triglyceride lowering and, surprisingly, significant reductions in plasma glucose and insulin. Halofenate is a selective PPAR-γ modulator (SPPARγM). SPPARγMs are believed to bind in distinct manners to the ligand-binding pocket of PPAR-γ, leading to altered receptor conformational stability and resulting in distinct patterns of gene expression. Thus, was suggested that halofenate hold promising therapeutic potential in the treatment of type 2 diabetes, without the side effects. However, information about the current use of this compound is not available.

Milipertine was studied in patients with severe schizophrenia. Information about the current use of the drug is not available.

Chloracyzine is phenothiazine derivative with vasodilatory activity. Chloracyzine produced a decrease in myocardial oxygen consumption accompanied by a reduction in coronary blood flow preceded by transient coronary dilatation. Chloracyzine produced an insignificant increase in arterial pressure; heart rate increased slightly in the open-chest experiments but not in the isolated heart. It is suggested that reduced oxygen uptake after chloracyzine is realized through improved efficiency in the use of oxygen.

Fluocinolone participated in clinical trials for the treatment of Oral Lichen Planus and Candida Infection.

Clomegestone (clomagestone) is an investigational steroidal progestogen. Clomegestone exhibits anti-estrogenic activity in estrone stimulated immature mice when administered orally at 100 ug.